MAPPICINE ANALOGS, INTERMEDIATES IN THE SYNTHESIS OF MAPPICINE ANALOGS AND METHODS OF SYNTHESIS OF MAPPICINE ANALOGS

摘要

A compound having the following structure: (I) wherein Z is -CHOR<1>R<2 >or -C(O)R<2>; R<1> is H, an alkyl group, an aryl group, -OC(O)OR, wherein R is an alkyl group, -C(O)R wherein R is an alkyl group, an aryl group, an alkoxy group, an amino group, an alkylamino group, a dialkylamino group, an aryl amino group, a diarylamino group, an arylalkyl amino group, a protecting group or a fluorous tag; R<2> is an alkyl group, an aryl group or an arylalkyl group; R<3> is H, an alkyl group, hydroxyalkyl group or an aryl group; R<4>-R<8> are independently the same or different and are hydrogen, an alkyl group, an alkenyl group, an alkynyl group, an aryl group, an alkoxy group, an aryloxy group, an acyloxy group, a haloalkyl group, a perfluoroalkyl group, fluorine, chlorine, bromine, a haloalkyloxy group, a carbamoyloxy group, a hydroxy group, a nitro group, a cyano group, a cyanoalkyl group, an azido group, an azidoalkyl group, a formyl group, a hydrazino group, a hydrazinoalkyl group, a hydroxyalkyl group, an alkoxyalkyl group, -NR<1>R, wherein R<1> and R are independently hydrogen, an alkyl group, an aryl group, an arylalkyl group, or -C(O)R, an aminoalkyl group, an alkylaminoalkyl group, a dialkylaminoalkyl group, an aryl aminoalkyl group, a diarylaminoalkyl group, an arylalkyl aminoalkyl group, -OC(O)OR, wherein R is an alkyl group, -C(O)R, -SR, S(O)R or S(O2)R wherein R is hydrogen, -C(O)R, an alkyl group, or an aryl group, (CH2)nSiRRR wherein n is an integer within the range of 0 through 10 and R, R and R are independently a C1-10 alkyl group, a C2-10 alkenyl group, a C2-10 alkynyl group, an aryl group, a haloalkyl group, a cyanoalkyl group, an azidoalkyl group, a hydrazinoalkyl group, a hydroxyalkyl group, an alkoxyalkyl group, an aminoalkyl group, an alkylaminoalkyl group, a dialkylaminoalkyl group, an aryl aminoalkyl group, a diarylaminoalkyl group, an arylalkyl aminoalkyl group. Alternatively R<4> and R<5>, R<6> and R<6>; R<6> and R<7>; or R<7> and R<8> can form together a chain of 3 or four groups selected from CH, CH2, O, S, N, NH, N-alkyl or N-aryl. Provided that, at least one of R<5>-R<7> is not H, a lower alkyl group, fluorine, a cyano group, a hydroxyl group, hydroxyalkyl group, an alkoxy group, an aminoalkyl group, an alkylaminoalkyl group, a dialkylaminoalkyl group, an amino group, an alkylamino group, a dialkylamino group, a carbamoyloxy group, a formyl group or -C(O)R wherein R is an alkyl group.